scholarly journals Biodistribution and pharmacokinetic studies on topically delivered technetium-99m-labeled 5-FU nanogel formulation for management of pre-cancerous skin lesions

2021 ◽  
Vol 18 (9) ◽  
pp. 1977-1983
Author(s):  
R. Rajagopalan ◽  
Sanjay K. Jain ◽  
Ankur Kaul ◽  
Piyush Trivedi
Keyword(s):  
High Stability ◽  
Entrapment Efficiency ◽  
Skin Lesions ◽  
Maximum Activity ◽  
Gamma Scintigraphy ◽  
Pharmacokinetic Studies ◽  
Site Specific ◽  
Technetium 99M ◽  
Low Intensity ◽  
Biodistribution Studies

Purpose: To prepare technetium-99m (99mTc)-labelled nanogel loaded with 5-fluorouracil (5-FU) containing synthesized gallic acid-stearylamine (GA-SA) conjugate in order to reduce its systemic toxicity and provide site-specific delivery to skin lesions. Methods: Lipid nanocarrier-based 1 % (w/w) 5-FU nanogel containing GA-SA conjugate was successfully formulated. Parameters that included pH, viscosity and entrapment efficiency were measured. Furthermore, 1 % (w/w) 5-FU nanogel and 1 % (w/w) 5-FU commercial formulations were radiolabelled with 99mTc. The radiolabelled 99mTc-5-FU nanogel and commercial formulations were subjected to successive preclinical assessments with respect to radiochemical stability, biodistribution, and gamma scintigraphy in BALB/c mice, and pharmacokinetic studies in New Zealand albino rabbits. Results: The entrapment efficiency of 5-FU in the nanogel preparation was 82.12 ± 1.2 %. The 5-FU nanogel formulation exhibited excellent radiolabelling efficiency (> 93 %) and high stability. Skin/blood localization ratios of 274.93 and 167.89 were obtained for topical radiolabelled drug-loaded 5-FU nanogel formulation and 5-FU commercial formulation, respectively, after 1 h of administration. Gamma scintigraphy and biodistribution studies showed that topically administered 99mTc-5-FU nanogel was distributed mostly in skin, when compared to marketed 5-FU formulation. Pharmacokinetic studies revealed low maximum activity in the blood (Cmax = 34.20 µg/mL), with low intensity (AUC) for topically administered 99mTc-5-FU nanogel formulation. Conclusion: 5-FU nanogel enhances specific delivery of 5-FU at targeted sites and decreases its toxicity in tissues distant from the site of application. The results suggest that nanogel loaded with 5-FU containing synthesized GA-SA conjugate is a novel effective approach for the treatment of skin lesions.

A novel d-glucose derivative radiolabeled with technetium-99m: Synthesis, biodistribution studies and scintigraphic images in an experimental model of Ehrlich tumor

2010 ◽  
Vol 20 (8) ◽  
pp. 2478-2480 ◽  
Author(s):  
André Luís Branco de Barros ◽  
Valbert Nascimento Cardoso ◽  
Luciene das Graças Mota ◽  
Elaine Amaral Leite ◽  
Mônica Cristina de Oliveira ◽  
...  
Keyword(s):  
Experimental Model ◽  
Ehrlich Tumor ◽  
Technetium 99M ◽  
Biodistribution Studies ◽  
Glucose Derivative

scholarly journals Preparation of crotalus venom radiolabeled with technetium-99m as a tool for biodistribution study

2005 ◽  
Vol 48 (spe2) ◽  
pp. 9-12 ◽  
Author(s):  
Priscilla Brunelli Pujatti ◽  
Carlos Jorge Rodrigues Simal ◽  
Raquel Gouvêa dos Santos
Keyword(s):  
Biological Activity ◽  
High Efficiency ◽  
High Yield ◽  
Clinical Use ◽  
Crude Venom ◽  
Technetium 99M ◽  
Biodistribution Studies ◽  
Nuclear Medicine Procedures ◽  
Distribution Studies ◽  
Exogenous Source

Technetium-99m (99mTc) has been the radionuclide of choice for nuclear medicine procedures and experimental research. Because of its optimal nuclear properties, 99mTc is suitable for high efficiency detection with the advantage of reduced radiological waste. Crotalus venom (CV) has been shown to reduce tumors in clinical studies and tissue distribution studies are very important for clinical use. The goal of this work was to obtain CV labeled with 99mTc which preserves its biological activity. After labeling, biological activity was assessed by hemolytic activity evaluation. Labeled and crude venom caused indirect hemolysis provided that the incubation medium contained an exogenous source of lecithin. High yield radiolabeled-CV was obtained and biological activity was preserved. The results suggest that 99mTc-CV can be a useful tool for biodistribution studies.

Enhanced oral bioavailability of nisoldipine-piperine-loaded poly-lactic-co-glycolic acid nanoparticles

2017 ◽  
Vol 6 (6) ◽  
pp. 517-526 ◽  
Author(s):  
Permender Rathee ◽  
Anjoo Kamboj ◽  
Shabir Sidhu
Keyword(s):  
Oral Bioavailability ◽  
Drug Loading ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Pharmacokinetic Interaction ◽  
Precipitation Method ◽  
Pharmacokinetic Studies ◽  
Average Particle

AbstractBackground:Piperine helps in the improvement of bioavailability through pharmacokinetic interaction by modulating metabolism when administered with other drugs. Nisoldipine is a substrate for cytochrome P4503A4 enzymes. The study was undertaken to assess the influence of piperine on the pharmacokinetics and pharmacodynamics of nisoldipine nanoparticles in rats.Methods:Optimization studies of nanoparticles were performed using Taguchi L9 orthogonal array, and the nanoparticles were formulated by the precipitation method. The influence of piperine and nanoparticles was evaluated by means of in vivo kinetic and dynamic studies by oral administration in rats.Results:The entrapment efficiency, drug loading, ζ potential, and average particle size of optimized nisoldipine-piperine nanoparticles was 89.77±1.06%, 13.6±0.56%, −26.5 mV, and 132±7.21 nm, respectively. The in vitro release in 0.1 n HCl and 6.8 pH phosphate buffer was 96.9±0.48% and 98.3±0.26%, respectively. Pharmacokinetic studies showed a 4.9-fold increase in oral bioavailability and a >28.376±1.32% reduction in systemic blood pressure by using nanoparticles as compared to control (nisoldipine suspension) in Wistar rats.Conclusion:The results revealed that piperine being an inhibitor of cytochrome P4503A4 enzymes enhanced the bioavailability of nisoldipine by 4.9-fold in nanoparticles.

scholarly journals Prospects of using extremely low doses of physical factors impact in food biotechnology

2018 ◽  
Vol 6 (2) ◽  
pp. 305-313 ◽  
Author(s):  
Tatiana Danilchuk ◽  
Tatiana Danilchuk ◽  
Vera Ganina ◽  
Vera Ganina
Keyword(s):  
Hydrolytic Enzymes ◽  
Physical Factor ◽  
Maximum Activity ◽  
Physical Factors ◽  
Experimental Sample ◽  
Low Doses ◽  
Resource Saving ◽  
Food Biotechnology ◽  
Low Intensity ◽  
Biotechnological Processes

The paper deals with urgent issues of development of resource-saving methods of biotechnological processes intensification. The main purpose of the work is to show the efficiency of using extremely low doses of physical factors impact in food biotechnology. Acoustic and electric treatment was in various modes. Impact capacity did not exceed 10-4 W/kg. The duration of exposure ranged from 5 to 15 min. Barley grains enzymes and lactic acid microorganisms were subjected to treatment. Impact of vibration as a physical factor, its frequency is considered as a priority in controlling growth and biochemical processes in biological objects. Impact frequency in the range of 50–10000 Hz influences the activity of hydrolytic enzymes in bimodal way. It is presented in the article. The coincidence of the frequency ranges of the maximum activity of enzymes in the model reactions with the ones in the grain of barley under the treatment of alternating current and sound is noted. Improvement of all indexes of germinating barley and improvement of the quality of the finished malt were observed in these ranges. Low-intensity acoustic treatment at a frequency of 2000 Hz contributed to an increase in β-galactosidase activity of the CT-95 Str. thermophilus strain. Selected ST-95 Str. thermophilus strain was used in the starter composition for the experimental sample production of fermented melted milk. The fermentation process intensification was observed. The lactose content of this product is 30% less in comparison with the feedstock. The use of traditional starter without a selected strain can reduce the lactose content by an average of 7.5%. The results of biotechnological processes modification by means of the treatment of enzymes and extremely low doses of physical factors impact used in meat technologies are observed. Thus, the prospects of using low-intensity physical effects of vibration in the development of innovative food technologies are substantiated. It is also promising to use these technologies in making absolutely new food products with different qualities.

Effects of low intensity laser irradiation during healing of infected skin lesions in the rat

2006 ◽  
Author(s):  
Ethne L. Nussbaum ◽  
Lothar Lilge ◽  
Tony Mazzulli ◽  
Kenneth P. Pritzker
Keyword(s):  
Laser Irradiation ◽  
Skin Lesions ◽  
Low Intensity ◽  
Intensity Laser ◽  
Infected Skin

scholarly journals FORMULATION AND EVALUATION OF METFORMIN HYDROCHLORIDE LOADED FLOATING MICROSPHERES

2019 ◽  
pp. 74-82
Author(s):  
SHIKHA KESHARVANI ◽  
PANKAJ KUMAR JAISWAL ◽  
ALOK MUKERJEE ◽  
AMIT KUMAR SINGH
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Release Kinetics ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Compatibility Study ◽  
Specific Drug ◽  
Site Specific

Objective: The main objective of this study was to develop and evaluate the eudragit and HPMC coated metformin hydrochloride floating microspheres, in which HPMC helps in floating and eudragit as a coating material for a site-specific drug release in a controlled manner and the active moiety metformin used as anti-hyperglycemic agent. Methods: The floating microsphere was prepared by the solvent evaporation method incorporating metformin as a model drug. The prepared floating microsphere were characterized for particle size, %yield, drug loading and entrapment efficiency, compatibility study, %buoyancy, surface morphology and In vitro drug release and release kinetics. Results: The result metformin loaded floating microsphere was successfully prepared and the particle size range from 397±23.22 to 595±15.82 µm, the entrapment efficiency range from 83.49±1.33 to 60.02±1.65% and drug loading capacity range from 14.3±0.54 to 13.31±0.47% and %buoyancy range from 85.67±0.58 to 80.67±1.15%. The FT-IR and X-RD analysis confirmed that no any interaction between drug and excipient, and surface morphology confirmed those particles are sphere. The floating microsphere show maximum 96% drug release in pH 0.1N HCL and follow the Korsmeyer peppas model of the super case-2 transport mechanism. Conclusion: These results suggest that metformin loaded floating microspheres could be retain in stomach for long time and give site specific drug release in controlled manner.

scholarly journals Boosting the Brain Delivery of Atazanavir through Nanostructured Lipid Carrier-Based Approach for Mitigating NeuroAIDS

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1059
Author(s):  
Saif Ahmad Khan ◽  
Saleha Rehman ◽  
Bushra Nabi ◽  
Ashif Iqubal ◽  
Nida Nehal ◽  
...  
Keyword(s):  
Targeted Delivery ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Fold Increase ◽  
Pharmacokinetic Studies ◽  
Nanostructured Lipid Carrier ◽  
Brain Delivery ◽  
The Brain

Atazanavir (ATZ) presents poor brain availability when administered orally, which poses a major hurdle in its use as an effective therapy for the management of NeuroAIDS. The utilization of nanostructured lipid carriers (NLCs) in conjunction with the premeditated use of excipients can be a potential approach for overcoming the limited ATZ brain delivery. Methods: ATZ-loaded NLC was formulated using the quality by design-enabled approach and further optimized by employing the Box–Behnken design. The optimized nanoformulation was then characterized for several in vitro and in vivo assessments. Results: The optimized NLC showed small particle size of 227.6 ± 5.4 nm, high entrapment efficiency (71.09% ± 5.84%) and high drug loading capacity (8.12% ± 2.7%). The release pattern was observed to be biphasic exhibiting fast release (60%) during the initial 2 h, then trailed by the sustained release. ATZ-NLC demonstrated a 2.36-fold increase in the cumulative drug permeated across the rat intestine as compared to suspension. Pharmacokinetic studies revealed 2.75-folds greater Cmax in the brain and 4-fold improvement in brain bioavailability signifying the superiority of NLC formulation over drug suspension. Conclusion: Thus, NLC could be a promising avenue for encapsulating hydrophobic drugs and delivering it to their target site. The results suggested that increase in bioavailability and brain-targeted delivery by NLC, in all plausibility, help in improving the therapeutic prospects of atazanavir.

Effects of low intensity laser irradiation during healing of skin lesions in the rat

2009 ◽  
Vol 41 (5) ◽  
pp. 372-381 ◽  
Author(s):  
Ethne L. Nussbaum ◽  
Tony Mazzulli ◽  
Kenneth P.H. Pritzker ◽  
Facundo Las Heras ◽  
Fang Jing ◽  
...  
Keyword(s):  
Laser Irradiation ◽  
Skin Lesions ◽  
Low Intensity ◽  
Intensity Laser

scholarly journals Glycosylation profiles determine extravasation and disease-targeting properties of armed antibodies

2015 ◽  
Vol 112 (7) ◽  
pp. 2000-2005 ◽  
Author(s):  
Dario Venetz ◽  
Christian Hess ◽  
Chia-wei Lin ◽  
Markus Aebi ◽  
Dario Neri
Keyword(s):  
Recombinant Protein ◽  
Tumor Targeting ◽  
Process Development ◽  
Negative Impact ◽  
Molecular Targets ◽  
Clear Correlation ◽  
Therapeutic Activity ◽  
Endothelial Lining ◽  
Site Specific ◽  
Biodistribution Studies

The ability of antibodies to extravasate out of blood vessels is critical for therapeutic activity, because molecular targets for most diseases are located outside of the endothelial lining. By performing detailed biodistribution studies with a novel IL9-armed cancer-specific antibody, we identified a clear correlation between N-linked glycan structures and tumor-targeting efficiencies. Site-specific glycan analysis provided a detailed view of the glycan microheterogeneity present on the IL9 portion of the recombinant protein. Nonsialylated glycan structures have a negative impact on disease-homing activity, highlighting the importance of glycosylation control and characterization during process development.

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